The present invention is various novel analogs of xanthine. Additionally, the invention is pharmaceutical compositions having as the active compound the novel analogs of xanthines. The invention is also methods of use of the analogs. The use of the analogs of the present invention relates particularly to a desirable affinity at adenosine receptors, particularly the A.sub.1 receptor. That is, the analogs are adenosine receptor antagonists. Thus, the analogs, for example, provide activity for use as a CNS stimulant, cognition activator, and bronchodilator.
Xanthines and particularly alkyl derivatives thereof, having adenosine receptor affinity are well known for use to treat cardiovascular diseases, as bronchodilators, and/or as psychotropic agents and CNS stimulants, as well as diuretics, and for the treatment of migraines or allergies.
More recently dialkenyl derivatives of xanthines are also found to have activity as adenosine antagonists. See copending U.S. Ser. No. 864,939 filed May 20, 1986, now abandoned.
The copending Application No. 885,057 filed July 14, 1986 which is a continuation in part of U.S. Ser. No. 864,939 filed May 20, 1986 now abandoned is hereby incorporated by reference having a review of related references also appropriate in the present invention. However, neither the copending U.S. Ser. No. 864,939 nor the references cited therein make obvious to one of ordinary skill a combination of substituents of the analogs of the present invention.